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Table 2 The binding affinities of toxin BmKKx2 towards wild-type and mutant hERG channel

From: Open conformation of hERG channel turrets revealed by a specific scorpion toxin BmKKx2

hERG mutant

IC50a

nb

IC50(mut)/IC50(wt)

 

nM

  

Wild Type

6.7 ± 1.7

7

1.0

H578A

N.Ec

5

-e

D580A

L.Ed

5

-

R582A

76.5 ± 32.6

4

11.4

I583A

87.5 ± 16.8

4

13.1

W585A

N.E

6

-

L586A

24.3 ± 8.4

4

3.6

H587A

59.7 ± 31.7

5

8.9

N588A

14.5 ± 4.3

4

2.2

L589A

L.E

6

-

D591A

19.6 ± 1.7

4

2.9

Q592A

89.5 ± 39.8

5

13.4

K595A

65.2 ± 19.1

5

9.7

P596A

60.8 ± 23.4

4

9.1

Y597A

118.2 ± 26.7

4

17.6

N598A

15.2 ± 4.8

4

2.3

S600A

12.1 ± 3.5

4

1.8

K608A

116.1 ± 29.2

5

17.3

D609A

L.E.

8

-

K610A

6.7 ± 5.1

5

1.0

T613A

42.6 ± 17.1

5

6.4

N629A

L.E

7

-

S631A

698.0 ± 64.4

5

104.2

  1. aIC50 value(half-maximum inhibition concentration) represents as Mean ± Standard Error.
  2. bnumber of independent experiments.
  3. cno expression, can’t detect fluorescent flag in all transfected HEK 293 T cells.
  4. dlow expression, with detectable fluorescent flag but can only elicit weak current in all transfected HEK 293 cells.
  5. e- means the lack of IC50 value of mutants.